In the quest to address unmet needs in treatment and prevention of various diseases in humans and other subjects, one avenue is the discovery of small organic molecules having potent biological activity. This process relies, in part, on the investigation of diverse chemical compounds, or libraries of compounds. In particular, the emphasis of investigation of stereochemical variation as it relates to biological activity, for instance agonism or antagonism of various receptor targets having implications in disease mechanisms, is ever increasing.
Stereodiverse nonpeptide ligands are one approach to the discovery of new therapeutic agents. Based on known peptide ligands to a particular target, the approach involves discovery of “peptide mimics” (or peptidomimetics), compounds that structurally mimic the peptide ligand in particular functions, but that are not peptides. As such, the nonpeptides can offer therapeutic advantages, such as improved selectivity to targets, improved bioavailability, lessened adverse side effects, ease of manufacture, etc.